Bulk Inquiry
TAK 063
- Soluble in DMSO
- MF: C23H17FN6O2
- MW: 428.42
Description
Highly potent, and orally active PDE10A inhibitor (IC50 value 0.30 nM) with excellent selectivity (>15000-fold selective over other PDEs). TAK-063 represents a promising drug for the treatment of schizophrenia with potential for superior safety and tolerability profiles.
More Information
| Parent CAS No. | 1238697-26-1 |
|---|---|
| Chemical Name | 1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one |
| SMILES | C1(C2N(C3=CC=CC=C3)N=CC=2)=NN(C2=CC=C(N3C=CC=N3)C=C2F)C=C(OC)C1=O |
| MFCD | N.A. |
| InChi | InChI=1S/C23H17FN6O2/c1-32-21-15-29(19-9-8-17(14-18(19)24)28-13-5-11-25-28)27-22(23(21)31)20-10-12-26-30(20)16-6-3-2-4-7-16/h2-15H,1H3 |
| InChiKey | KVHRYLNQDWXAGI-UHFFFAOYSA-N |
| CID | 46848915 |
| Short Description | PDE10A inhibitor |
References
- J. Kunitomo et al. Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active PDE10A inhibitor. J Med Chem. 2014 Nov 26;57(22):9627-43.
- K. Suzuki et al. In vivo pharmacological characterization of TAK-063, a potent and selective phosphodiesterase 10A inhibitor with antipsychotic-like activity in rodents. J Pharmacol Exp Ther. 2015 Mar;352(3):471-9.
- A. Harada et al. Characterization of binding and inhibitory properties of TAK-063, a novel phosphodiesterase 10A inhibitor. PLoS One. 2015 Mar 27;10(3):e0122197.
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